Perspectives
| Covalent Modifiers: An Orthogonal Approach to Drug Design Michele H. Potashman and Mark E. Duggan 1231-1246  |
| Full: PDF (981 K) |
Letters
| Discovery of Novel Myc−Max Heterodimer Disruptors with a Three-Dimensional Pharmacophore Model Gabriela Mustata, Ariele Viacava Follis, Dalia I. Hammoudeh, Steven J. Metallo, Huabo Wang, Edward V. Prochownik, John S. Lazo and Ivet Bahar 1247-1250  |
| Full: PDF (372 K) |
| Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily Gretchen M. Schroeder, Yongmi An, Zhen-Wei Cai, Xiao-Tao Chen, Cheryl Clark, Lyndon A. M. Cornelius, Jun Dai, Johnni Gullo-Brown, Ashok Gupta, Benjamin Henley, John T. Hunt, Robert Jeyaseelan, Amrita Kamath, Kyoung Kim, Jonathan Lippy, Louis J. Lombardo, Veeraswamy Manne, Simone Oppenheimer, John S. Sack, Robert J. Schmidt, Guoxiang Shen, Kevin Stefanski, John S. Tokarski, George L. Trainor, Barri S. Wautlet, Donna Wei, David K. Williams, Yingru Zhang, Yueping Zhang, Joseph Fargnoli and Robert M. Borzilleri 1251-1254  |
| Full: PDF (1059 K) |
| Discovery of (R)-6-Cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a Potent and Orally Available Hepatitis C Virus Polymerase Inhibitor Hui Li, John Tatlock, Angelica Linton, Javier Gonzalez, Tanya Jewell, Leena Patel, Sarah Ludlum, Matthew Drowns, Sadayappan V. Rahavendran, Heather Skor, Robert Hunter, Stephanie T. Shi, Koleen J. Herlihy, Hans Parge, Michael Hickey, Xiu Yu, Fannie Chau, Jim Nonomiya and Cristina Lewis 1255-1258  |
| Full: PDF (275 K) |
| Anthracene Based Compounds as New L-type Ca2+ Channel Blockers: Design, Synthesis, and Full Biological Profile Sergio Bova, Simona Saponara, Angela Rampa, Silvia Gobbi, Lorenzo Cima, Fabio Fusi, Giampietro Sgaragli, Maurizio Cavalli, Cristobal de los Rios, Jorg Striessnig and Alessandra Bisi 1259-1262  |
| Full: PDF (147 K) |
Articles
| Detection of Metabolite Changes in C6 Glioma Cells Cultured with Antimitotic Oleyl Glycoside by 1H MAS NMR Isabel Garcia-Alvarez, Leoncio Garrido, Ernesto Doncel-Perez, Manuel Nieto-Sampedro and Alfonso Fernandez-Mayoralas 1263-1267  |
| Full: PDF (130 K) |
| Syntheses and Antigestagenic Activity of Mifepristone Derivatives Claudia Hodl, Katrin Raunegger, Rainer Strommer, Gerhard F. Ecker, Olaf Kunert, Sonja Sturm, Christoph Seger, Ernst Haslinger, Rudolf Steiner, Wolfgang S. L. Strauss and Hans-Wolfgang Schramm 1268-1274  |
| Full: PDF (149 K) |
| Discovery of Imidazo[1,2-b]thiazole Derivatives as Novel SIRT1 Activators Chi B. Vu, Jean E. Bemis, Jeremy S. Disch, Pui Yee Ng, Joseph J. Nunes, Jill C. Milne, David P. Carney, Amy V. Lynch, Jesse J. Smith, Siva Lavu, Philip D. Lambert, David J. Gagne, Michael R. Jirousek, Simon Schenk, Jerrold M. Olefsky and Robert B. Perni 1275-1283  |
| Full: PDF (538 K) |
| 10-(2-oxo-2-Phenylethylidene)-10H-anthracen-9-ones as Highly Active Antimicrotubule Agents: Synthesis, Antiproliferative Activity, and Inhibition of Tubulin Polymerization Helge Prinz, Peter Schmidt, Konrad J. Bohm, Silke Baasner, Klaus Muller, Eberhard Unger, Matthias Gerlach and Eckhard G. Gunther 1284-1294  |
| Full: PDF (270 K) |
| Novel Pyrrolidine Ureas as C−C Chemokine Receptor 1 (CCR1) Antagonists J. Robert Merritt, Jinqi Liu, Elizabeth Quadros, Michelle L. Morris, Ruiyan Liu, Rui Zhang, Biji Jacob, Jennifer Postelnek, Catherine M. Hicks, Weiqing Chen, Earl F. Kimble, W. Lynn Rogers, Linda O’Brien, Nicole White, Hema Desai, Shalini Bansal, George King, Michael J. Ohlmeyer, Kenneth C. Appell and Maria L. Webb 1295-1301  |
| Full: PDF (132 K) |
| Nuclear Factor-κB Mediated Inhibition of Cytokine Production by Imidazoline Scaffolds Daljinder K. Kahlon, Theresa A. Lansdell, Jason S. Fisk, Christopher D. Hupp, Timothy L. Friebe, Stacy Hovde, A. Daniel Jones, Richard D. Dyer, R. William Henry and Jetze J. Tepe 1302-1309  |
| Full: PDF (141 K) |
| Structural Requirements for a Lipoamino Acid in Modulating the Anticonvulsant Activities of Systemically Active Galanin Analogues Liuyin Zhang, Charles R. Robertson, Brad R. Green, Timothy H. Pruess, H. Steve White and Grzegorz Bulaj 1310-1316  |
| Full: PDF (123 K) |
| Structure−Activity Relationships of Antitubercular Nitroimidazoles. 1. Structural Features Associated with Aerobic and Anaerobic Activities of 4- and 5-Nitroimidazoles Pilho Kim, Liang Zhang, Ujjini H. Manjunatha, Ramandeep Singh, Sejal Patel, Jan Jiricek, Thomas H. Keller, Helena I. Boshoff, Clifton E. Barry, and Cynthia S. Dowd 1317-1328  |
| Full: PDF (257 K) |
| Structure−Activity Relationships of Antitubercular Nitroimidazoles. 2. Determinants of Aerobic Activity and Quantitative Structure−Activity Relationships Pilho Kim, Sunhee Kang, Helena I. Boshoff, Jan Jiricek, Margaret Collins, Ramandeep Singh, Ujjini H. Manjunatha, Pornwaratt Niyomrattanakit, Liang Zhang, Michael Goodwin, Thomas Dick, Thomas H. Keller, Cynthia S. Dowd and Clifton E. Barry, 1329-1344  |
| Full: PDF (484 K) |
| Synthesis, Cytotoxicity, and DNA Interactions of New Cisplatin Analogues Containing Substituted Benzimidazole Ligands Fatma Gomus, Gokcen Eren, Leyla Acık, Ayten Celebi, Fatma Ozturk, Sukran Yılmaz, Rahsan Ilıkcı Sagkan, Sibel Gur, Aykut Ozkul, Ayhan Elmalı and Yalcın Elerman 1345-1357  |
| Full: PDF (1514 K) |
| Synthesis and in Vitro and in Vivo Evaluation of 18F-Labeled Positron Emission Tomography (PET) Ligands for Imaging the Vesicular Acetylcholine Transporter Zhude Tu, Simon M. N. Efange, Jinbin Xu, Shihong Li, Lynne A. Jones, Stanley M. Parsons and Robert H. Mach 1358-1369  |
| Full: PDF (637 K) |
| Second-Generation Highly Potent and Selective Inhibitors of the Hepatitis C Virus NS3 Serine Protease Kevin X. Chen, Latha Nair, Bancha Vibulbhan, Weiying Yang, Ashok Arasappan, Stephane L. Bogen, Srikanth Venkatraman, Frank Bennett, Weidong Pan, Melissa L. Blackman, Angela I. Padilla, Andrew Prongay, Kuo-Chi Cheng, Xiao Tong, Neng-Yang Shih and F. George Njoroge 1370-1379  |
| Full: PDF (394 K) |
| Derivatives of 5-Nitro-furan-2-carboxylic Acid Carbamoylmethyl Ester Inhibit RNase H Activity Associated with HIV-1 Reverse Transcriptase Hideyoshi Fuji, Emiko Urano, Yuko Futahashi, Makiko Hamatake, Junko Tatsumi, Tyuji Hoshino, Yuko Morikawa, Naoki Yamamoto and Jun Komano 1380-1387  |
| Full: PDF (997 K) |
| New Insights into the Design of Inhibitors of Human S-Adenosylmethionine Decarboxylase: Studies of Adenine C8 Substitution in Structural Analogues of S-Adenosylmethionine Diane E. McCloskey, Shridhar Bale, John A. Secrist, , Anita Tiwari, Thomas H. Moss, , Jacob Valiyaveettil, Wesley H. Brooks, Wayne C. Guida, Anthony E. Pegg and Steven E. Ealick 1388-1407  |
| Full: PDF (1206 K) |
| Candidate Selection and Preclinical Evaluation of N-tert-Butyl Isoquine (GSK369796), An Affordable and Effective 4-Aminoquinoline Antimalarial for the 21st Century Paul M. O’Neill, B. Kevin Park, Alison E. Shone, James L. Maggs, Phillip Roberts, Paul A. Stocks, Giancarlo A. Biagini, Patrick G. Bray, Peter Gibbons, Neil Berry, Peter A. Winstanley, Amira Mukhtar, Richard Bonar-Law, Stephen Hindley, Ramesh B. Bambal, Charles B. Davis, Martin Bates, Timothy K. Hart, Stephanie L. Gresham, Ron M. Lawrence, Richard A. Brigandi, Federico M. Gomez-delas-Heras, Domingo V. Gargallo and Stephen A. Ward 1408-1415  |
| Full: PDF (482 K) |
| Design, Synthesis, and Biological Evaluation of 6α- and 6β-N-Heterocyclic Substituted Naltrexamine Derivatives as μ Opioid Receptor Selective Antagonists Guo Li, Lindsey C. Aschenbach, Jianyang Chen, Michael P. Cassidy, David L. Stevens, Bichoy H. Gabra, Dana E. Selley, William L. Dewey, Richard B. Westkaemper and Yan Zhang 1416-1427  |
| Full: PDF (1659 K) |
| Synthesis and Evaluation of 18F-Labeled 2-Phenylbenzothiazoles as Positron Emission Tomography Imaging Agents for Amyloid Plaques in Alzheimer’s Disease Kim Serdons, Christelle Terwinghe, Peter Vermaelen, Koen Van Laere, Hank Kung, Luc Mortelmans, Guy Bormans and Alfons Verbruggen 1428-1437  |
| Full: PDF (359 K) |
| A New Class of Vitamin D Analogues that Induce Structural Rearrangement of the Ligand-Binding Pocket of the Receptor Yuka Inaba, Nobuko Yoshimoto, Yuta Sakamaki, Makoto Nakabayashi, Teikichi Ikura, Hirokazu Tamamura, Nobutoshi Ito, Masato Shimizu and Keiko Yamamoto 1438-1449  |
| Full: PDF (1841 K) |
| A Basis for Reduced Chemical Library Inhibition of Firefly Luciferase Obtained from Directed Evolution Douglas S. Auld, Ya-Qin Zhang, Noel T. Southall, Ganesha Rai, Marc Landsman, Jennifer MacLure, Daniel Langevin, Craig J. Thomas, Christopher P. Austin and James Inglese 1450-1458  |
| Full: PDF (1514 K) |
| 2-Acetylpyridine Thiosemicarbazones are Potent Iron Chelators and Antiproliferative Agents: Redox Activity, Iron Complexation and Characterization of their Antitumor Activity Des R. Richardson, Danuta S. Kalinowski, Vera Richardson, Philip C. Sharpe, David B. Lovejoy, Mohammad Islam and Paul V. Bernhardt 1459-1470  |
| Full: PDF (793 K) |
| Synthesis and Evaluation of Vancomycin Aglycon Analogues That Bear Modifications in the N-Terminal d-Leucyl Amino Acid Christine M. Crane and Dale L. Boger 1471-1476  |
| Full: PDF (357 K) |
Brief Articles
| Enantioselectivity in Cardioprotection induced by (S)- (−)-2,2-Dimethyl-N-(4′-acetamido-benzyl)-4-spiromorpholone-chromane Simona Rapposelli, Vincenzo Calderone, Roberto Cirilli, Maria Digiacomo, Cristina Faggi, Francesco La Torre, Mariaelisa Manganaro, Alma Martelli and Lara Testai 1477-1480  |
| Full: PDF (397 K) |
| Synthesis, Biological Evaluation, and Docking Studies of N-Substituted Acetamidines as Selective Inhibitors of Inducible Nitric Oxide Synthase Cristina Maccallini, Antonia Patruno, Neva Besker, Jamila Isabella Ali, Alessandra Ammazzalorso, Barbara De Filippis, Sara Franceschelli, Letizia Giampietro, Mirko Pesce, Marcella Reale, Maria L. Tricca, Nazzareno Re, Mario Felaco and Rosa Amoroso 1481-1485  |
| Full: PDF (413 K) |
| Structure−Activity Relationship of New Anti-Hepatitis C Virus Agents: Heterobicycle−Coumarin Conjugates Johan Neyts, Erik De Clercq, Raghunath Singha, Yung Hsiung Chang, Asish R. Das, Subhasish K. Chakraborty, Shih Ching Hong, Shwu-Chen Tsay, Ming-Hua Hsu and Jih Ru Hwu 1486-1490  |
| Full: PDF (120 K) |
Book Reviews
| Book Review of Dopamine Transporters: Chemistry, Biology, and Pharmacology Trent J. Volz 1491-1491 |
| Full: PDF (32 K) |
| Book Review of Natural Compounds as Drugs. Volumes 1 and 2 Mark T. Hamann 1491-1492 |
| Full: PDF (32 K) |